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<dc:creator>Rubio Antolin, Ana Rosa</dc:creator>
<dc:creator>González, Rocío</dc:creator>
<dc:creator>Busto Vázquez, Natalia</dc:creator>
<dc:creator>Vaquero Gutiérrez, Mónica</dc:creator>
<dc:creator>Iglesias, Ana L.</dc:creator>
<dc:creator>Jalón Sotés, Félix Ángel</dc:creator>
<dc:creator>Espino Ordóñez, Gustavo</dc:creator>
<dc:creator>Rodríguez, Ana M.</dc:creator>
<dc:creator>García Ruiz, Begoña</dc:creator>
<dc:creator>Manzano, Blanca R. .</dc:creator>
<dc:date>2021-09</dc:date>
<dc:description>An important challenge in the field of anticancer chemotherapy is the search for new species&#xd;
to overcome the resistance of standard drugs. An interesting approach is to link bioactive ligands to&#xd;
metal fragments. In this work, we have synthesized a set of p-cymene-Ru or cyclopentadienyl-M&#xd;
(M = Rh, Ir) complexes with four chrysin-derived pro-ligands with different -OR substituents at&#xd;
position 7 of ring A. The introduction of a piperidine ring on chrysin led to the highly cytotoxic&#xd;
pro-ligand HL4 and its metal complexes L4-M (SW480 and A549 cell lines, cytotoxic order: L4-Ir >&#xd;
L4-Ru ≈ L4-Rh). HL4 and its complexes induce apoptosis and can overcome cis-platinum resistance.&#xd;
However, HL4 turns out to be more cytotoxic in healthy than in tumor cells in contrast to its metal&#xd;
complexes which displayed higher selectivity than cisplatin towards cancer cells. All L4-M complexes&#xd;
interact with double stranded DNA. Nonetheless, the influence of the metal is clear because only&#xd;
complex L4-Ir causes DNA cleavage, through the generation of highly reactive oxygen species (1O2&#xd;
).&#xd;
This result supports the hypothesis of a potential dual mechanism consisting of two different chemical&#xd;
pathways: DNA binding and ROS generation. This behavior provides this complex with a great&#xd;
effectivity in terms of cytotoxicity</dc:description>
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<dc:identifier>http://hdl.handle.net/10259/6825</dc:identifier>
<dc:language>eng</dc:language>
<dc:publisher>MDPI</dc:publisher>
<dc:title>Anticancer Activity of Half-Sandwich Ru, Rh and Ir Complexes with Chrysin Derived Ligands: Strong Effect of the Side Chain in the Ligand and Influence of the Metal</dc:title>
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